TAK-259
TAK-259 is an orally active and selective α1D adrenoceptor (α1D-AR) antagonist with a Ki value of 1.1 nM. TAK-259 inhibits excessive contraction of bladder smooth muscle and prolongs voiding intervals. TAK-259 is promising for research of urinary system diseases[1][2].
Product Specifications
CAS Number
1192348-73-4
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H335
Target
Adrenergic Receptor
Related Pathways
GPCR/G Protein; Neuronal Signaling
Field of Research
Endocrinology
Smiles
O=C(C1=CC(Cl)=CN(CC2=CC(Cl)=CC=C2S(=O)(C)=O)C1=N)N
Molecular Formula
C14H13Cl2N3O3S
Molecular Weight
374.24
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P362+P364-P405-P501
References & Citations
[1]Sato A, et al. Structure determination, synthesis, and biological evaluation of a metabolite of the selective α1D adrenoceptor antagonist TAK-259[J]. Tetrahedron, 2016, 72 (41) : 6334-6339.|[2]Sakauchi N, et al. Discovery of 5-Chloro-1- (5-chloro-2- (methylsulfonyl) benzyl) -2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. J Med Chem. 2016 Apr 14;59 (7) :2989-3002.
Shipping Conditions
Room temperature
Scientific Category
Reference compound2
Clinical Information
No Development Reported
Isoform
α adrenergic receptor
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